Patent US4729985A successfully refreshed from Google Patents.
US4729985A
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Renin inhibitors containing 5-amino-2,5-disubstituted-4-hydroxypentanoic acid residues
Assignee: Pfizer Inc
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Filing: 1986-04-30
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Granted: 1988-03-08
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Expires: 2006-04-30
Abstract
Abstract A series of novel polypeptide derivatives, containing 5-amino-2,5-disubstituted-4-hydroxypentanoic acid residues, which are useful for inhibiting the angiotensinogen-cleaving action of the enzyme renin. Particularly valuable precursors for many of these compounds are certain other 5-amino-2,5-disubstituted-4-hydroxypentanoic acid derivatives.
Inventors
- 👤 Edward F. Kleinman
- 👤 Robert L. Rosati
- 👤 Jasjit S. Bindra
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 10:32
CPC Classifications
C; C07; C07K; C07K7/00; C07K7/04; C07K7/14; C07D; C07D307/00; C07D307/02; C07D307/26; C07D307/30; C07D307/32; C07D307/33; A; A61; A61P; A61P43/00; A61P9/00; A61P9/12; C07C; C07C271/00; C07C271/06; C07C271/08; C07C271/10; C07C271/22; C07D207/00; C07D207/02; C07D207/04; C07D207/10; C07D207/16; C07D217/00; C07D217/02; C07D217/06; C07D405/00; C07D405/02; C07D405/12; C07K5/00; C07K5/02; C07K5/0227; Y; Y10; Y10S; Y10S530/00; Y10S530/86
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
114 words
A polypeptide derivative of the formula ##STR22## or a pharmaceutically acceptable salt thereof, wherein ##STR23## R is hydrogen or an amino protecting acyl group having a molecular weight of less than 500; R 1 and R 2 are each independently hydrogen, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkenyl, phenyl, naphthyl, (C 4 -C 7 )cycloalkyl, (C 4 -C 7 )cycloalkenyl, (C 7 -C 9 )phenylalkyl, (C 11 -C 13 ) naphthylalkyl or (C 5 -C 10 ) (cycloalkyl)alkyl; and Y is OR 9 or NR 9 R 10 ; where R 9 and R 10 are each independently hydrogen, (C 1 -C 5 )alkyl, (C 4 -C 7 )cycloalkyl or benzyl.
Claim 2
Dependent Claim
114 words
A polypeptide derivative of the formula ##STR22## or a pharmaceutically acceptable salt thereof, wherein ##STR23## R is hydrogen or an amino protecting acyl group having a molecular weight of less than 500; R 1 and R 2 are each independently hydrogen, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkenyl, phenyl, naphthyl, (C 4 -C 7 )cycloalkyl, (C 4 -C 7 )cycloalkenyl, (C 7 -C 9 )phenylalkyl, (C 11 -C 13 ) naphthylalkyl or (C 5 -C 10 ) (cycloalkyl)alkyl; and Y is OR 9 or NR 9 R 10 ; where R 9 and R 10 are each independently hydrogen, (C 1 -C 5 )alkyl, (C 4 -C 7 )cycloalkyl or benzyl.
Claim 3
Dependent Claim
9 words
A compound of claim 1 wherein R is t-butyloxycarbonyl.
Claim 4
Dependent Claim
9 words
A compound of claim 2 wherein Y is OH.
Claim 5
Dependent Claim
10 words
A compound of claim 3 wherein R 1 is cyclohexylmethyl.
Claim 6
Dependent Claim
10 words
The compound of claim 4 wherein R 2 is isopropyl.
Claim 7
Dependent Claim
24 words
A pharmaceutical composition containing a renin inhibiting-effective amount of a compound of claim 1 as the essential active ingredient in a pharmaceutically acceptable carrier.
Claim 8
Dependent Claim
24 words
A pharmaceutical composition containing a renin inhibiting-effective amount of a compound of claim 2 as the essential active ingredient in a pharmaceutically acceptable carrier.
Claim 9
Dependent Claim
24 words
A pharmaceutical composition containing a renin inhibiting-effective amount of a compound of claim 3 as the essential active ingredient in a pharmaceutically acceptable carrier.
Claim 10
Dependent Claim
24 words
A pharmaceutical composition containing a renin inhibitin-effective amount of a compound of claim 4 as the essential active ingredient in a pharmaceutically acceptable carrier.
Claim 11
Dependent Claim
23 words
A pharmaceutical composition containing a renin inhibiting-effective amount of a compound of claim 5 as the essential active ingredient in a pharmaceutical carrier.
Claim 12
Dependent Claim
31 words
A method for inhibiting the cleavage of angiotensinogen by renin in the body of a mammal which comprises administering to the mammal an effective amount of a compound of claim 1.
Claim 13
Dependent Claim
31 words
A method for inhibiting the cleavage of angiotensinogen by renin in the body of a mammal which comprises administering to the mammal an effective amount of a compound of claim 2.
Claim 14
Dependent Claim
34 words
In a method for inhibiting the cleavage of angiotensinogen by renin in the body of a mammal which comprises administering orally to the mammal a renin-inhibiting effective amount of a compound of claim 3.
Claim 15
Dependent Claim
31 words
A method for inhibiting the cleavage of angiotensinogen by renin in the body of a mammal which comprises administering to the mammal an effective amount of a compound of claim 4.
Claim 16
Dependent Claim
31 words
A method for inhibiting the cleavage of angiotensinogen by renin in the body of a mammal which comprises administering to the mammal an effective amount of a compound of claim 5.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1991-03-08 | 1991-09-07 | 1992-03-08 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-03-08 | 1995-09-07 | 1996-03-08 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-03-08 | 1999-09-07 | 2000-03-08 | $7700.00 | Window Closed / Lapsed |